کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5826635 | 1558892 | 2016 | 21 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Preventive and alleviative effects of the dual enkephalinase inhibitor (Denki) PL265 in a murine model of neuropathic pain
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کلمات کلیدی
DRGAPNPSNLPWLS.E.M.DOPPKCintracerebroventricularMOPi.c.v.CCIp.o.Per os - per oschronic constrictive injury - آسیب مغزی کمرنگAminopeptidase N - آمینوپپتیداز NEndogenous enkephalins - انکهفالین های اندوژنTolerance - تلرانس standard error of the mean - خطای استاندارد میانگینNeuropathic pain - درد نوروپاتیکBBB - سد خونی مغزیBlood-brain barrier - مانع خون مغزیNEP - نپNeprilysin - نپریلینProtein kinase C - پروتئین کیناز سیPrevention - پیشگیریMu opioid receptor - گیرنده اپیدمی مdelta opioid receptor - گیرنده دلتا اپیوئید
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Preventive and alleviative effects of the dual enkephalinase inhibitor (Denki) PL265 in a murine model of neuropathic pain Preventive and alleviative effects of the dual enkephalinase inhibitor (Denki) PL265 in a murine model of neuropathic pain](/preview/png/5826635.png)
چکیده انگلیسی
Neuropathic pain remains difficult to treat due to the involvement of various pathophysiological mechanisms in its pathogeny. Among the different opioidergic systems the enkephalinergic one is primarily recruited via activation of delta opioid receptor (DOP) in chronic pain and of mu opioid receptor (MOP) in acute pain. To investigate the role of their endogenous ligands Met and Leu-enkephalin in neuropathic pain control, a dual inhibitor of their degrading enzymes, PL265, which acts restrictively at the level of peripheral nociceptors, was administered per os to assess its efficacy in pain prevention and alleviation using a partial sciatic nerve ligation model (PSNL) in mice. We demonstrated here that the pre-injury oral administration of PL265 (50Â mg/kg) during the 9 days of neuropathy development reduces thermal hyperalgesia and mechanical allodynia for two weeks after the end of treatment. The repeated administration (50Â mg/kg daily, during 10 days) does not induce tolerance. Therefore, protecting the enkephalins released at the peripheral level during neuropathic pain with oral PL265 seems to be a promising approach to prevent and alleviate the painful symptoms of neuropathic pain in humans without the unwanted effects of exogenous opiates such as morphine.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 788, 5 October 2016, Pages 176-182
Journal: European Journal of Pharmacology - Volume 788, 5 October 2016, Pages 176-182
نویسندگان
Elisabeth Bonnard, Hervé Poras, Marie-Claude Fournié-Zaluski, Bernard P. Roques,